Lipophilic molecules, such as nutrients and vitamins, are poorly solubilized in the aqueous medium along the gastrointestinal tract, thereby leading to poor bioavailability. These nutrients, including Coenzyme Q10, vitamins A, D, E and K, lycopene, lutein, resveratrol, and others, are not readily absorbed by body due to this poor solubility in an aqueous medium, i.e., the gastrointestinal fluid. The compromised bioavailability of these nutrients would be mitigated by solubility-enhancing technologies that can increase their bioavailability and efficacy. Various attempts have been made to solve this problem.
For example, U.S. Pat. No. 6,045,826 discloses water-soluble compositions containing a lipophilic compound (including CoQ10) and a single solubilizing agent having both hydrophobic and hydrophilic moieties.
Formulations useful for delivery of a particular exemplary beneficial agent, coenzyme Q (CoQ10) are described in the art. U.S. Pat. No. 7,438,903 notes that softgels are the most popular method of CoQ10 delivery, and CoQ10 is available commercially in the form of tablets, hard capsules and softgel capsules either alone or in combination with other vitamins and/or supplements. U.S. Pat. No. 4,483,873 discloses aqueous solutions of CoQ10 that contain hydrogenated lecithin putatively to increase CoQ10 bioavailability. U.S. Pat. Nos. 6,056,971, 6,441,050 and 7,094,804 disclose methods for solubilizing water-insoluble dietary supplements in liquid form, such as CoQ10 in a softgel, by mixing CoQ10 with, among other things, an edible polyhydric alcohol solvent. U.S. Pat. No. 6,300,377 teaches the formulation of a CoQ10 composition that omits polyhydric alcohol, but includes other agents to help improve solubility, including a glyceryl ester molecule having one to three C2-C7 acyl groups. WO/2005/111224 discloses CoQ10 complexes with beta-cyclodextrin to increase CoQ10 solubility in water.
U.S. Pat. No. 7,273,624 describes a melt extrusion process to prepare a CoQ10 solid dispersion in a matrix-forming excipient. U.S. Pat. No. 7,438,903 discloses CoQ10 nano-crystals dispersed in lipid-based carriers.
WO 00/38655A-1 describes formulations comprising porous calcium hydrogen phosphate particulates, sold commercially under the trademark Fujicalin®, within which a liquid formulation of an active agent is absorbed, so that the liquid-absorbing particulates can be processed using conventional pharmaceutical equipment. These formulations are said to provide high concentrations of active drug dosage without loss of active pharmaceutical agent during the manufacturing process, and to permit delivery of active pharmaceutical agent, along with suitable solubilization-enhancers to the absorption site. Other forms of the porous particulates are also disclosed including microcrystalline cellulose, silicon dioxide, or magnesium aluminosilicate, or blends thereof. However, this publication does not disclose incorporation of a supersaturated solution (SSS) of drug or a self-emulsifying formulation (SEF) of a drug so as to prevent reprecipitation.